Total control: The antibiotic BE‐43472B with a unique bisanthraquinone structure has been synthesized in a completely stereocontrolled manner. The key steps are 1) a pinacol rearrangement to install the angular naphthyl group, 2) a diastereoselective methylation of a lactol derivative, and 3) the late‐stage installation of the labile hydroxy group through an epoxide.